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Author: Frank Kozielski, FSB
Publisher: Springer
ISBN: 9401797323
Category : Medical
Languages : en
Pages : 276
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Book Description
This interdisciplinary volume collates research work on kinesins and cancer. Authors attempt to validate members of the kinesin superfamily as potential targets for drug development in cancer chemotherapy. The work begins by highlighting the importance of kinesins, summarising current knowledge and how they are shown to be crucial for mitosis. Chapters go on to explore how this family of proteins are emerging as a novel target for chemotherapeutic intervention and drug development. Readers will learn how kinesins travel along microtubules to fulfill their many roles in intracellular transport or cell division. Several compounds that inhibit two mitotic kinesins (called Eg5 and CENP-E) have entered Phase I and II clinical trials and are explored in these chapters. Additional mitotic kinesins are currently being validated as drug targets, raising the possibility that the repertoire of kinesin-based drug targets may expand in the future. The book is suitable as a reference standard for the field of kinesins and cancer. It will interest those in academia and pharmaceutical companies, and anyone with an interest in the medical relevance of these proteins, which cutting edge methodologies are now enabling us to understand in astonishing detail.
Author: Frank Kozielski, FSB
Publisher: Springer
ISBN: 9401797323
Category : Medical
Languages : en
Pages : 276
Get Book Here
Book Description
This interdisciplinary volume collates research work on kinesins and cancer. Authors attempt to validate members of the kinesin superfamily as potential targets for drug development in cancer chemotherapy. The work begins by highlighting the importance of kinesins, summarising current knowledge and how they are shown to be crucial for mitosis. Chapters go on to explore how this family of proteins are emerging as a novel target for chemotherapeutic intervention and drug development. Readers will learn how kinesins travel along microtubules to fulfill their many roles in intracellular transport or cell division. Several compounds that inhibit two mitotic kinesins (called Eg5 and CENP-E) have entered Phase I and II clinical trials and are explored in these chapters. Additional mitotic kinesins are currently being validated as drug targets, raising the possibility that the repertoire of kinesin-based drug targets may expand in the future. The book is suitable as a reference standard for the field of kinesins and cancer. It will interest those in academia and pharmaceutical companies, and anyone with an interest in the medical relevance of these proteins, which cutting edge methodologies are now enabling us to understand in astonishing detail.
Author: Qian
Publisher:
ISBN: 9780470290729
Category : Kinesin
Languages : en
Pages : 400
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Book Description
Playing a key role in cell function and transport, mitotic kinesins are a promising drug target in cancer and other diseases. Featuring contributions from editors and authors on the frontlines of kinesin drug discovery, Targeting Mitotic Kinesins in Drug Discovery covers the fundamentals, approaches, and current clinical status of drugs targeting mitotic kinesins. This comprehensive resource provides pharmaceutical scientists, medicinal chemists, biochemists, pharmacologists, structural and cell biologists, and researchers with in-depth coverage of the medicinal chemistry, biochemistry, and cell biology of agents targeting mitotic kinesins.
Author: Meredith C. Henderson
Publisher:
ISBN:
Category :
Languages : en
Pages : 246
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Book Description
UA62784 is a novel fluorenone identified in a biologic screen of compounds that are selectively cytotoxic in DPC4 (deleted in pancreatic cancer)-deleted pancreatic cancer cells. We sought to determine the mechanism of action of UA62784, and discovered it to be a potent mitotic inhibitor. UA62784 affects the ATPase activity of the mitotic kinesin centromere protein E (CENP-E), but does not affect other known mitotic kinesins. This inhibition of ATPase activity is not caused by an inhibition of microtubule binding nor is it caused by a failure of the kinesin to translocate to the nucleus during mitosis. Despite the anti-cancer properties of this drug, UA62784 is relatively insoluble and is not suitable as a lead compound for further development. Once we determined the mechanism of action of UA62784, we sought to determine if analogs would demonstrate the same potent mitotic inhibition while also offering properties such as increased solubility. A small library of chemical analogs was generated wherein each compound was a slight variation of UA62784 (termed the DPC series). Several potential leads were identified which exhibited increased solubility and/or increased cytotoxic activity. When tested for CENP-E ATPase inhibition, some compounds were noted to inhibit other kinesins as well. We therefore created a screen where each of the DPC compounds was tested for activity in Eg5, CENP-E, MKLP-1, MCAK, and KIF3C kinesins. Within these data, there is a correlation between cellular IC50 and kinesin ATPase inhibition for CENP-E and MKLP-1. A few compounds emerged from these studies, including DPC046, which has a low cellular IC50 and inhibits all five kinesins to some degree. DPC046 was used in a mouse xenograft study to determine in vivo efficacy, but no significant tumor shrinkage was seen, likely due to solubility limitations affecting theamount of bioavailable compound. From these studies we conclude that the cytotoxic effects seen in UA62784 and its analogs are due, at least in part, to their inhibition of kinesin proteins. We demonstrate that compounds that inhibit CENP-E and other kinesin proteins hold promise in cytotoxically targeting pancreatic cancer cells. Further development is needed to optimize DPC046 compound solubility in order to increase in vivo efficacy.
Author: Caterina A. M. La Porta
Publisher: Cambridge University Press
ISBN: 1108150330
Category : Science
Languages : en
Pages : 187
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Book Description
Recent years have witnessed an increasing number of theoretical and experimental contributions to cancer research from different fields of physics, from biomechanics and soft-condensed matter physics to the statistical mechanics of complex systems. Reviewing these contributions and providing a sophisticated overview of the topic, this is the first book devoted to the emerging interdisciplinary field of cancer physics. Systematically integrating approaches from physics and biology, it includes topics such as cancer initiation and progression, metastasis, angiogenesis, cancer stem cells, tumor immunology, cancer cell mechanics and migration. Biological hallmarks of cancer are presented in an intuitive yet comprehensive way, providing graduate-level students and researchers in physics with a thorough introduction to this important subject. The impact of the physical mechanisms of cancer are explained through analytical and computational models, making this an essential reference for cancer biologists interested in cutting-edge quantitative tools and approaches coming from physics.
Author: Claire T. Friel
Publisher: CRC Press
ISBN: 0429958242
Category : Medical
Languages : en
Pages : 132
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Book Description
This book brings together current information on the families that make up the kinesin superfamily of molecular motors in one comprehensive text; an ideal reference for researchers looking to make comparisons between different families, for specific information on an individual family, or simply for an overview of the kinesin superfamily. Information is clearly structured and grouped according to individual families and organised in a standardised way, allowing the reader to easily search and retrieve information on this large superfamily of molecular motors and understand how its individual members carry out a diverse variety of cellular functions. Features : The first book dedicated to the entire kinesin superfamily Enables a fuller understanding of this family of proteins, which is becoming an increasing focus of research due to its involvement in diseases such as cancer, neuropathies and ciliopathies Written in a manner accessible to a range of researchers in the life and medical sciences, including biophysicists, biochemists and medical researchers. Chapters 4 and 11 of this book are freely available as downloadable Open Access PDFs at http://www.taylorfrancis.com under a Creative Commons Attribution-Non Commercial-No Derivatives (CC-BY-NC-ND) 4.0 license.
Author: Bruce Alberts
Publisher:
ISBN: 9780815332183
Category : Cytology
Languages : en
Pages : 0
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Book Description
Author: Stephen M. King
Publisher: Academic Press
ISBN: 0123820049
Category : Science
Languages : en
Pages : 657
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Book Description
Research on dyneins has a direct impact on human diseases, such as viruses and cancer. With an accompanying website showing over 100 streaming videos of cell dynamic behavior for best comprehension of material, Dynein: Structure, Biology and Disease is the only reference covering the structure, biology and application of dynein research to human disease. From bench to bedside, Dynein: Structure, Biology and Disease offers research on fundamental cellular processes to researchers and clinicians across developmental biology, cell biology, molecular biology, biophysics, biomedicine, genetics and medicine. Broad-based up-to-date resource for the dynein class of molecular motors Chapters written by world experts in their topics Numerous well-illustrated figures and tables included to complement the text, imparting comprehensive information on dynein composition, interactions, and other fundamental features
Author:
Publisher: Academic Press
ISBN: 0080957188
Category : Science
Languages : en
Pages : 3533
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Book Description
Biophysics is a rapidly-evolving interdisciplinary science that applies theories and methods of the physical sciences to questions of biology. Biophysics encompasses many disciplines, including physics, chemistry, mathematics, biology, biochemistry, medicine, pharmacology, physiology, and neuroscience, and it is essential that scientists working in these varied fields are able to understand each other's research. Comprehensive Biophysics, Nine Volume Set will help bridge that communication gap. Written by a team of researchers at the forefront of their respective fields, under the guidance of Chief Editor Edward Egelman, Comprehensive Biophysics, Nine Volume Set provides definitive introductions to a broad array of topics, uniting different areas of biophysics research - from the physical techniques for studying macromolecular structure to protein folding, muscle and molecular motors, cell biophysics, bioenergetics and more. The result is this comprehensive scientific resource - a valuable tool both for helping researchers come to grips quickly with material from related biophysics fields outside their areas of expertise, and for reinforcing their existing knowledge. Biophysical research today encompasses many areas of biology. These studies do not necessarily share a unique identifying factor. This work unites the different areas of research and allows users, regardless of their background, to navigate through the most essential concepts with ease, saving them time and vastly improving their understanding The field of biophysics counts several journals that are directly and indirectly concerned with the field. There is no reference work that encompasses the entire field and unites the different areas of research through deep foundational reviews. Comprehensive Biophysics fills this vacuum, being a definitive work on biophysics. It will help users apply context to the diverse journal literature offering, and aid them in identifying areas for further research Chief Editor Edward Egelman (E-I-C, Biophysical Journal) has assembled an impressive, world-class team of Volume Editors and Contributing Authors. Each chapter has been painstakingly reviewed and checked for consistent high quality. The result is an authoritative overview which ties the literature together and provides the user with a reliable background information and citation resource
Author:
Publisher: Academic Press
ISBN: 0128029420
Category : Medical
Languages : en
Pages : 345
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Book Description
Advances in Cancer Research provides invaluable information on the exciting and fast-moving field of cancer research. Here, once again, outstanding and original reviews are presented on a variety of topics, including taxane-anti-androgens cross-resistance in advanced prostate cancer and proteasome inhibitors in the treatment of multiple myeloma. Provides information on cancer research Outstanding and original reviews Suitable for researchers and students
Author: Alexander E. Knight
Publisher: Academic Press
ISBN: 008092123X
Category : Science
Languages : en
Pages : 369
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Book Description
Single molecule techniques, including single molecule fluorescence, optical tweezers, and scanning probe microscopy, allow for the manipulation and measurement of single biological molecules within a live cell or in culture. These approaches, amongst the most exciting tools available in biology today, offer powerful new ways to elucidate biological function, both in terms of revealing mechanisms of action on a molecular level as well as tracking the behaviour of molecules in living cells. This book provides the first complete and authoritative treatment of this rapidly emerging field, explicitly from a biological perspective.The contents are organized by biological system or molecule. Each chapter discusses insights that have been revealed about their mechanism, structure or function by single molecule techniques. Among the topics covered are enzymes, motor proteins, membrane channels, DNA, ribozymes, cytoskeletal proteins, and other key molecules of current interest. An introduction by the editor provides a concise review of key principles and an historical overview. The last section discusses applications in molecular diagnostics and drug discovery. Organized by biological system or molecule Each chapter discusses insights into mechanism of action, structure, and function Covers enzymes, motor proteins, membrane channels, DNA, ribozymes, etc Includes an introduction to key principles and an historical overview Discusses applications in molecular diagnostics and drug discovery Provides an expert's perspective on future development
